Nitrogen In Substituent Q Patents (Class 564/86)
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Patent number: 6271419Abstract: The present invention relates to a process and a reagent useful for the synthesis of sulphanilide which is perhalogenated on the carbon borne by the sulphur atom of the sulphanilide function. This persulphonylation process is characterized in that it comprises a step of placing a nucleophile, whose nucleophilic atom is a nitrogen, in contact with a reagent comprising, for successive or simultaneous addition, a heavy halide of sulphonyl, advantageously sulphonyl chloride, and an organic base comprising a trivalent atom from column V whose lone pair is conjugated directly or indirectly to a bond, and in that the organic part of the said sulphonyl is perhalogenated, advantageously perfluorinated, on the carbon borne by the sulphur. Application to the synthesis of intermediates for organic chemistry.Type: GrantFiled: November 4, 1999Date of Patent: August 7, 2001Assignee: Rhodia ChimieInventors: Jean-Roger Desmurs, André Millet, Virginie Pevere
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Patent number: 6271263Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.Type: GrantFiled: March 2, 1999Date of Patent: August 7, 2001Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Benjamin Sklarz, Ramy Lidor, Eliezer Bahar, Yaacov Herzig, Jeff Sterling, Alex Veinberg
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Patent number: 6258852Abstract: Disclosed are methods for treating or preventing inflammatory bowel disease (IBD) using aryl nitrone compounds. Pharmaceutical compositions containing aryl nitrone compounds which are useful for the treatment or prophylaxis of IBD are also disclosed.Type: GrantFiled: May 8, 2000Date of Patent: July 10, 2001Assignee: Centaur Pharmaceuticals, Inc.Inventors: William D. Flitter, William A. Garland, Beverly Greenwood Van-Meerveld, Ian Irwin
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Patent number: 6251827Abstract: Acylsulfamoylbenzamides of the formula I and crop protection compositions comprising them are described. In this formula I, R1, R2, R3, R4 and R5 are various organic radicals and X is CH or N.Type: GrantFiled: September 25, 1998Date of Patent: June 26, 2001Assignee: Hoechst Schering AgrEvo GmbHInventors: Frank Ziemer, Lothar Willms, Thomas Auler, Hermann Bieringer, Christopher Rosinger
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Patent number: 6248785Abstract: This invention relates to novel compounds, pharmaceutical compositions comprising these compounds and their use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: January 22, 1999Date of Patent: June 19, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine L. Widdowson, John Gerald Gleason
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Patent number: 6221866Abstract: in which R(1) to R(8) have the meanings stated in the claims, act on the Kv1.5 potassium channel, and inhibit a potassium current, referred to as “ultra-rapidly activating delayed rectifier,” in the human atrium. They are therefore very particularly suitable as novel antiarrhythmic active substances, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g., atrial fibrillation or atrial flutter.Type: GrantFiled: June 23, 2000Date of Patent: April 24, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Uwe Gerlach, Hans Ulrich Stilz, Hans-Jochen Lang
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Patent number: 6221914Abstract: The present invention is directed to compounds which are capable of inhibiting the activity of tryptase. Such compounds are useful in the treatment or prevention of inflammatory disease, particularly those disease states which are mediated by mast cell activation. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds and methods for treating or preventing an inflammatory disease.Type: GrantFiled: October 27, 1998Date of Patent: April 24, 2001Assignee: Array Biopharma Inc.Inventors: Laurence E. Burgess, James P. Rizzi
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Patent number: 6214882Abstract: Benzenesulphonamide compounds of general formula (I), wherein R1 is a hydrogen or halogen atom such as chlorine or fluorine, or a straight or branched C1-4 alkyl or C1-4 alkoxy group, each of R2, R3 and R4, which are the same or different, is a hydrogen atom or a straight, branched or cyclic C1-4 alkyl group, and R1 is a hydrogen atom or a C1-2 alkyl, C1-2 fluoroalkyl or C1-2 perfluoroalkyl group, in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures, as well as pharmaceutically acceptable acid addition salts thereof, are provided for therapeutical use.Type: GrantFiled: January 16, 1998Date of Patent: April 10, 2001Assignee: SynthelaboInventors: Thomas Purcell, Christophe Philippo
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Patent number: 6211241Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.Type: GrantFiled: June 1, 1998Date of Patent: April 3, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
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Patent number: 6191170Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: January 7, 1999Date of Patent: February 20, 2001Assignee: Tularik Inc.Inventor: Julio C. Medina
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Patent number: 6174922Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: February 23, 1999Date of Patent: January 16, 2001Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Dennis Michael Zimmerman, Ana Maria Escribano
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Patent number: 6169116Abstract: Compounds of formula I wherein R1, R2, R3, R4 and R5 are as defined in the description, are useful as pharmaceuticals.Type: GrantFiled: June 28, 1999Date of Patent: January 2, 2001Assignee: Novartis AGInventor: Robert Swoboda
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Patent number: 6133315Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: March 16, 1999Date of Patent: October 17, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6103766Abstract: Compounds of Formula I and their pharmaceutically acceptable salts having selective dopamine D3 receptor activity suitable for treating central nervous system disorders. Formula I: ##STR1## R.sub.1 is independently H or a C.sub.1 -C.sub.8 alkyl including isomeric forms thereof;R.sub.2 is H, C.sub.1 -C.sub.3 alkyl, a halogen, OCH.sub.3 , OCF.sub.3, CF.sub.3, CN, SCH.sub.3 or NHCOCH.sub.3 ; andR.sub.3 is H, C.sub.1 -C.sub.3 alkyl, a halogen, OCH.sub.3 , OCF.sub.3, CF.sub.3, CN, SCH.sub.3 or NHCOCH.sub.3.Type: GrantFiled: May 7, 1999Date of Patent: August 15, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Arthur Glenn Romero, Jeffrey A. Leiby
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Patent number: 6096930Abstract: The present invention relates to novel cyclohexane-1-3-dione derivatives of formula (1) useful as herbicides and plant-growth regulants, ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkyl, nitro, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, C.sub.1 -C.sub.6 sulfamoyl, and N, N-di(C.sub.1 -C.sub.6 alkyl)sulfamoyl group; (X)n represents the number of X substituents which may be substituted on benzene ring, wherein n is 1, 2 or 3. Also, cyclohexyl moiety, one of the substituents on benzofuran ring, is substituted at C-4, C-5, C-6 or C-7 position on benzene ring; R.sup.1 is selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl group; R.sup.2 is selected from the group consisting of C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl and C.sub.2 -C.sub.6 alkynyl group; R.sup.3 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.Type: GrantFiled: May 12, 1998Date of Patent: August 1, 2000Assignee: Korea Research Institute of Chemical TechnologyInventors: Eung Kul Ryu, Kyoung Mahn Kim, Jae Nyoung Kim, Jin Seog Kim
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Patent number: 6096924Abstract: One object of the invention is a process for the catalytic hydrogenation of aromatic nitro compounds in solution or in melt in the presence of hydrogen and at least one noble metal catalyst, nickel catalyst or cobalt catalyst, in which process a catalytic amount of at least one vanadium compound is present, wherein the vanadium has the oxidation state 0, II, IV or V. It has been found that in the catalytic hydrogenation of aromatic nitro compounds the accumulation of hydroxylamines can be almost completely prevented by the addition of catalytic amounts of vanadium compounds, which usually results in concentrations of <1% hydroxylamine. The resulting hydrogenated products are whiter (purer) than those obtained without the addition of the vanadium compound because almost no azo or azoxy compounds are obtained. The hydrogenation, in particular the final phase, proceeds faster than without said addition. Accordingly, substantial advantages with respect to quality constancy and economy are obtained.Type: GrantFiled: November 13, 1997Date of Patent: August 1, 2000Assignee: Novartis AGInventors: Martin Studer, Peter Baumeister
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Patent number: 6090981Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(ozy)yl, E is O or S; Y is --[CR(3).sub.2 ].sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z in Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.Type: GrantFiled: May 19, 1998Date of Patent: July 18, 2000Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David W. Laufer
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Patent number: 6075166Abstract: The present invention is to novel photochemically cleavable aryl sulfonamides of the formulaP--A.sub.3 --A.sub.2 --A.sub.1 --S(O).sub.2 NR.sub.1 R.sub.2whereinR.sub.1 and R.sub.2 are independently selected from optionally substituted alkyl, arylalkyl or heteroarylalkyl;A.sub.1 is an aryl or heteroaryl moiety;A.sub.2 is a linking agent is an aryl, heteroaryl, arylalkyl, heteroaryl alkyl, or an alkyl, wherein the alkyl moiety in the arylalkyl, heteroaryl alkyl, or alkyl group is optionally interrupted one or more times independently by oxygen, NR.sub.3, sulfur or an amide group;R.sub.3 is alkyl;A.sub.3 is an electron rich aryl or heteroaryl moiety having an E.sub.1/2 potential of 0.5 to 2.0 and which moiety is capable of forming an exciplex;P is a solid support.Another aspect of the present invention is to the novel use of these photolytically cleavable aryl sulfonamides in combinatorial chemistry synthesis, for use in non-sequential encoding, as a tagging agent.Type: GrantFiled: March 31, 1995Date of Patent: June 13, 2000Assignee: SmithKline Beecham CorporationInventors: Ravi Shunker Garigipati, Jerry Leroy Adams
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Patent number: 6060491Abstract: The present application describes 6-membered aromatics of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein D may be CH.sub.2 NH.sub.2 or C(.dbd.NH)NH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: June 18, 1998Date of Patent: May 9, 2000Assignee: Dupont PharmaceuticalsInventors: James Russell Pruitt, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Ruth Richmond Wexler
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Patent number: 6057322Abstract: Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.Type: GrantFiled: July 30, 1997Date of Patent: May 2, 2000Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 6037377Abstract: Compounds of the formula ##STR1## which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.Type: GrantFiled: June 5, 1995Date of Patent: March 14, 2000Assignee: Boehringer Ingelheim KGInventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Frank Himmelsbach, Franz Birke, Armin Fugner
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Patent number: 6034067Abstract: The invention relates to a compound having formula (I), wherein A, B, X, N, Z and Q are defined as described in the description. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-related diseases.Type: GrantFiled: August 12, 1998Date of Patent: March 7, 2000Assignee: Akzo Nobel, N.V.Inventors: Peter Diederik Jan Grootenhuis, Adrianus Petrus Antonius de Man, Anton Egbert Peter Adang
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Patent number: 6001881Abstract: Benzoylguanidines of the formula I ##STR1## in which: R(1) to R(4) have the meanings given in the claims, are antiarrhythmic pharmaceuticals, having a cardioprotective component, which are also valuable for the prevention of ischemically induced damage, in particular in association with the triggering of ischemically induced cardiac arrhythmias. As a consequence of inhibiting the cellular Na.sup.+ /H.sup.+ exchange mechanism, they are used for treating acute or chronic damage triggered by ischemia. In addition to this, they are notable for their strong inhibitory effect on the proliferation of cells. They are suitable for preventing the genesis of high blood pressure.Type: GrantFiled: June 4, 1997Date of Patent: December 14, 1999Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
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Patent number: 5998665Abstract: The present invention is concerned with compounds of formula I ##STR1## wherein Z, R.sup.1 and R.sup.2 are as defined herein, as well as their pharmaceutically acceptable salts as therapeutically active substances against central nervous system disorders and for the production of corresponding medicaments.Type: GrantFiled: June 3, 1998Date of Patent: December 7, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Claus Riemer, Andrew Sleight
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Patent number: 5994398Abstract: Arylsulfonamides which have the general structure: with the symbols R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and n representing the groups and integers provided in the detailed description are provided herein. These compounds have activity as inhibitors of phospholipase A2, inhibitors of cytokine release and as inhibitors of neurodegeneration.Type: GrantFiled: December 11, 1996Date of Patent: November 30, 1999Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Russell E. Rydel, Eugene D. Thorsett
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Patent number: 5968978Abstract: Compounds of the formula I ##STR1## in which the symbols have the meanings indicated in the claims, have outstanding antiarrhythmic properties. They exhibit a cardioprotective component. They can inhibit or greatly decrease, in a preventive manner, the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias. Moreover, they have a strong inhibitory action on the proliferation of cells.Type: GrantFiled: September 21, 1998Date of Patent: October 19, 1999Assignee: Hoechst Marion Roussel DeutschlandInventors: Heinz-Werner Kleemann, Jan-Robert Schwark, Sabine Faber, Hans Jochen Lang, Andreas Weichert, Hans-Willi Jansen
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Patent number: 5965588Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 26, 1998Date of Patent: October 12, 1999Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5955505Abstract: A method comprising administering a sulfonamide derivative to a patient requiring activation of glutamate receptors, the sulfonamide derivative represented by the formula ##STR1## wherein A is a napthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 40 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group, and an acetamido group, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group of --OCH.sub.2 -- or a group of --CH.dbd.CH--; X and Y are the same or different, and are each a hydrogen atom or a fluorine atom; R is a carboxy group, an alkoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of ##STR2## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and R.sub.Type: GrantFiled: August 20, 1997Date of Patent: September 21, 1999Assignee: Nippon Suisan Kaisha, Ltd.Inventors: Jiro Takeo, Shinya Yamashita, Keiji Wada, Yoshiyuki Chiba
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Patent number: 5945450Abstract: Naphthalene derivatives represented by formula ?I!: ##STR1## (wherein A is a hydrogen atom, a hydroxy group, a C.sub.7 -C.sub.11 aralkyloxy group, or an alkoxy group composed of an oxy group and a C.sub.1 -C.sub.12 aliphatic or alicyclic, saturated or unsaturated hydrocarbon group where the allyl may be substituted with a C.sub.6 -C.sub.10 allyloxy group; Q represents O, S, CH.sub.2, O--CH.sub.2, S--CH.sub.2, CO, or CHOR.sup.1 ; L represents CO, CR.sup.2 R.sup.3 CO, CH.sub.2 CH.sub.2 CO, or CH.dbd.CHCO; D represents a hydrogen atom, NO.sub.2, NH.sub.2, CO.sub.2 R.sup.4, or a group having the following formula ?II!: ##STR2## (wherein G represents. a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.6, CN, or a tetrazol-5-yl group); E represents a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.5, CN, or a tetrazol-5-yl group; M represents a hydrogen atom, a C.sub.1 -C.sub.4 lower alkyl group, a nitro group, or a halogen atom; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.Type: GrantFiled: November 22, 1996Date of Patent: August 31, 1999Assignee: Teijin LimitedInventors: Kazuya Takenouchi, Katsushi Takahashi, Masaichi Hasegawa, Takahiro Takeuchi, Keiji Komoriya
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Patent number: 5932195Abstract: Arylaminomethylenecamphor derivatives of the formula (1) ##STR1## where the C.dbd.C double bond is in the Z or E configuration, and the variables have the following meanings:R.sup.1 H, CH.sub.3,R.sup.2 H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.8 -cycloalkenyl, aryl or substituted aryl,R.sup.3 H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, aryl, substituted aryl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.8 -acyl,Ar aryl, substituted aryl, hetaryl or substituted hetaryl,are used as sunscreen agents, especially in cosmetic and pharmaceutical formulations.Type: GrantFiled: January 13, 1998Date of Patent: August 3, 1999Assignee: BASF AktiengesellschaftInventors: Michael Drogemuller, Volker Bomm, Volker Schehlmann, Horst Westenfelder
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Patent number: 5869725Abstract: Derivatives of gamma-amino-alpha,beta-unsaturated sulfonic acids, a process for the preparation of the same and their utilization in the synthesis of pseudopeptides characterized by the presence of at least a sulfonamide type bond conjugated to a double bond are described.Type: GrantFiled: October 30, 1996Date of Patent: February 9, 1999Assignee: Pharmacia & UpJohn S.P.A.Inventors: Cesare Gennari, Donatella Potenza, Barbara Salom
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Patent number: 5866611Abstract: Compounds of formula I, and their pharmaceutically acceptable salts, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR.sup.1 R.sup.2 is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthese and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.Type: GrantFiled: May 19, 1994Date of Patent: February 2, 1999Assignee: Zeneca LimitedInventors: George Robert Brown, Murdoch Allan Eakin, Peter John Harrison, deceased, Keith Blakeney Mallion
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Patent number: 5856479Abstract: Using the fluorescent group-containing carbodiimide compound represented-by the following formula (I) as the label and the like in the nucleic acid detection method, immunoassay, or chemiluminescence assay, labeling can be made efficiently for a short time, a nucleic acid derived from nature can be labelled, and highly sensitive assay is enabled.B--Y.sup.3 --N.dbd.C.dbd.N--Y.sup.2 --W--Y.sup.1 --?A!.sub.n --F(I)wherein F represents a fluorescent group;A represents a moiety selected from the group consisting of --CH.sub.2 --, --NHCO--, --CONH--, --O--, --S--, --NR-- wherein R is an alkyl group, --COO--, --OCO--, --NHSO.sub.2 --, and --SO.sub.2 NH--;n is 0 or 1;W represents a direct bond or a quaternary ammonium group;Y.sup.1, Y.sup.2 and Y.sup.3 each represents an alkylene group which may have a functional group in its main chain; andB represents H or a monovalent organic group which may be the same as or different from that represented by --W--Y.sup.1 --?A!.sub.n --F.Type: GrantFiled: May 16, 1997Date of Patent: January 5, 1999Assignee: Nisshinbo Industries, Inc.Inventors: Osamu Suzuki, Gen Masuda, Namiko Shiohata, Kazuko Matsumoto
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Patent number: 5814110Abstract: Distillate fuel is treated with additives whose structure match the crystal planes of the wax which crystallizes from the fuel to produce crystals below 4000 nanometres in size, suitable additive include novel sulpho-carboxylic materials particularly their esters and amine derivatives such as the amine salts and/or amides of ortho-sulpho benzoic acid.Type: GrantFiled: November 23, 1994Date of Patent: September 29, 1998Assignee: Exxon Chemical Patents Inc.Inventors: Kenneth William Bartz, Jacqueline Dawn Bland, David Paul Gillingham, Richard Dix Kerwood, Edwin William Lehmann, Kenneth Lewtas, John Edward Maddox, Albert Rossi, Robert Dryden Tack
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Patent number: 5776951Abstract: The present invention is concerned with diaryl compounds of formula (l) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.Type: GrantFiled: April 11, 1996Date of Patent: July 7, 1998Assignee: Glaxo Wellcome Inc.Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
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Patent number: 5763481Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.8 cycloalkyl, halo-C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, halo-C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, --Si(R.sub.3).sub.3, --S--R.sub.4, --SO.sub.2 --R.sub.6 or --CO--R.sub.9 ;R.sub.2 is halogen, C.sub.1 -C.sub.4 alkyl or CF.sub.3, the substituents R.sub.2 being identical or different when n is 2;R.sub.3 each independently of the others is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or phenyl;R.sub.4 is aryl or heteroaryl each of which is unsubstituted or substituted;R.sub.6 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.20 -alkoxy, C.sub.2 -C.sub.6 alkenyloxy, C.sub.2 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, aryl, aryloxy or arylthio, or is optionally substituted amino;R.sub.9 is hydroxy, unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.Type: GrantFiled: July 10, 1996Date of Patent: June 9, 1998Assignee: Novartis CorproationInventors: Peter Maienfisch, Manfred Boger, Thomas Pitterna, Henry Szczepanski
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Patent number: 5760064Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 6, 1997Date of Patent: June 2, 1998Assignee: G.D. SearleInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5753660Abstract: Selected sulfonylalkanoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: November 13, 1996Date of Patent: May 19, 1998Assignee: G. D. Searle & Co.Inventors: James A. Sikorski, Daniel P. Getman, Gary A. DeCrescenzo, Balekudru Devadas, John N. Freskos, Hwang-Fun Lu, Joseph J. McDonald
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Patent number: 5750661Abstract: Dyes of the formula ##STR1## where the ring A may be benzofused and R.sup.1 -R.sup.6 have the meaning defined in the specification, with the proviso that at least one quaternizable or quaternary group is present in the molecule; use of said dyes for dyeing or printing polymeric material, and novel amides of J-acid.Type: GrantFiled: August 30, 1996Date of Patent: May 12, 1998Assignee: BASF AktiengesellschaftInventors: Ulrike Schloesser, Udo Mayer
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Patent number: 5741819Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: ##STR1## or pharmaceutically acceptable salts thereof; whereinR.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R.sup.2 is one of hydrogen, alkyl, cycloalkyl or aryl; R.sup.3 is one of hydrogen, hydroxy or alkoxy; R.sup.4 is one of --NH.sub.2, phenyl or pyridyl, wherein said phenyl and said pyridyl are optionally substituted with one or two of halogen, hydroxy, hydroxyalkyl, alkoxy, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and/or dialkylaminoalkyl; X is one of --CH.sub.2 -- or --C(O)--; and n is from zero to eleven; provided that when R.sup.4 is --NH.sub.2, then R.sup.3 is hydrogen and n is other than zero; and also provided that when R.sup.Type: GrantFiled: June 7, 1995Date of Patent: April 21, 1998Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Carl R. Illig, Richard M. Soll, Joseph M. Salvino, Bruce E. Tomczuk, Tianbao Lu, Nalin L. Subasinghe
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Patent number: 5739166Abstract: A class of terphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and halo; or wherein R.sup.2 and R.sup.3 together form --OCH.sub.2 O--; wherein each of R.sup.6 through R.sup.8 is independently selected from hydrido, lower alkyl, halo, lower alkoxy, lower haloalkyl, and lower dialkylamino; or wherein R.sup.6 and R.sup.7 together form --OCH.sub.2 O; and wherein R.sup.12 is selected from lower alkylsulfonyl and aminosulfonyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: November 29, 1994Date of Patent: April 14, 1998Assignee: G.D. Searle & Co.Inventors: David B. Reitz, Jinglin Li, Monica B. Norton
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Patent number: 5736579Abstract: A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein n is a number selected from 0, 1 and 2; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: November 18, 1994Date of Patent: April 7, 1998Assignee: G.D. Searle & Co.Inventors: David B. Reitz, Robert E. Manning, Horng-Chi Huang, Jinglin Li
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Patent number: 5734081Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: June 1, 1995Date of Patent: March 31, 1998Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5716993Abstract: The present invention provides an anthranilic acid derivative having a cGMP-PDE inhibitory activity.An anthranilic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, a nitro group, a hydroxyalkyl group, a cyano group or the like; R.sup.5 and R.sup.6 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group or the like;W represents a group of the formula: --N.dbd. or --CH.dbd.; R.sup.7 and R.sup.Type: GrantFiled: September 14, 1995Date of Patent: February 10, 1998Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Keiji Ishibashi, Hironori Ikuta, Hiroki Ishihara, Shigeru Souda
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Patent number: 5708004Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: January 13, 1998Assignee: Monsanto CompanyInventors: John J. Talley, Kathryn L. Reed
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Patent number: 5705528Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein thyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: ##STR1## wherein R.sup.1 represents farnesyl, geranyl or geranyl-geranyl;Z represents C--R.sup.6 or N;R.sup.2 represents H, CN, the groups COOR.sup.7, SO.sub.3 R.sup.7, CONR.sup.7 R.sup.8 and SO.sub.2 NR.sup.7 R.sup.7, wherein R.sup.7 and R.sup.8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO.sub.3 M, wherein M is a cation;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato;X represents O, S, SO, SO.sub.2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.Type: GrantFiled: November 10, 1994Date of Patent: January 6, 1998Assignee: Ramot University Authority for Applied Research & Industrial DevelopmentInventor: Yoel Kloog
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Patent number: 5693672Abstract: 3,4,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing themBenzoylguanidines of the formula I ##STR1## where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, where R(4) and R(5) are alk(en)yl, --C.sub.n H.sub.2n --R(7), and where R(7) is cycloalkyl or phenyl, where R(5) is also H, R(6) is H or C.sub.1 --C.sub.4 --alkyl,R(2) is hydrogen, (cyclo)-alk(en)(yn)yl, aryl and hetaryl,R(3) is defined as R(2)and their pharmaceutically tolerable salts are described.Type: GrantFiled: May 26, 1995Date of Patent: December 2, 1997Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Hans-Jochen Lang, Wolfgang Scholz, Udo Albus, Florian Lang
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Patent number: 5670544Abstract: There are described benzoylguanidines of the formula I ##STR1## where R(1) is hydrogen, Hal, --NO.sub.2, --CN, --CF.sub.3, R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, where m is zero to 2, R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), n is zero to 4, where R(5) also has the meaning of H,R(6) is H or (C.sub.1 -C.sub.4)-alkyl, where R(5) and R(6) together can be 4 or 5 methylene groups,R(2) is --SR(10), --OR(10), --NRH(10), --NR(10)R(11), --CHR(10)R(12), ##STR2## where R(10) and R(11) are identical or different and are--?CHR(16)!.sub.s --(CH.sub.2).sub.p --(CHOH).sub.q --(CH.sub.2).sub.r --(CH.sub.2 OH).sub.t --R(21) or --(CH.sub.2).sub.p --O--(CH.sub.2 --CH.sub.2 O).sub.q --R(21)R(12) and R(13) are hydrogen or alkyl or, together with the carbon atom carrying them, form a cycloalkyl,R(14) is H, (cyclo)alkyl or --C.sub.n H.sub.2n --R(15),R(3) is defined as R(1), or is alkyl, hydrogen or --X--R(22) where X is oxygen, S or NR(16),and their pharmaceutically tolerable salts.Type: GrantFiled: May 26, 1995Date of Patent: September 23, 1997Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Hans-Jochen Lang, Heinz-Werner Kleemann, Wolfgang Scholz, Udo Albus
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Patent number: 5668178Abstract: Phenylthiols and dithiobisbenzamides are potent antibacterial and antiviral agents.Type: GrantFiled: May 19, 1995Date of Patent: September 16, 1997Assignee: Warner-Lambert CompanyInventors: Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5668291Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N, R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: June 7, 1995Date of Patent: September 16, 1997Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti